Cilastatin sodium

Product Name: Cilastatin sodium
CAS No.: 81129-83-1
Chemical Name: Cilastatin sodium
Synonyms: l642957;Cilastatine;Sodium Cilastatin;Cilastatin sodium;Cilastatin Impurity 9;Cilastatin sodium CRS;Cilastatin sodium (C2170000);Cilastatin sodium Ready Made Solution;Cilastatin for system suitability 2 CRS;Cilastatin for system suitability 1 CRS
CBNumber: CB8260633
Molecular Formula: C16H25N2O5S.Na
Formula Weight: 380.44
MOL File: 81129-83-1.mol

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Cilastatin sodium Property

Melting point:: >160°C (dec.)
Flash point:: 87℃
storage temp.: 2-8°C
solubility: Very soluble in water and in methanol, slightly soluble in anhydrous ethanol, very slightly soluble in dimethyl sulfoxide, practically insoluble in acetone and in methylene chloride.
form: Solid
pka: pKa1 2.0; pKa2 4.4; pKa3 9.2(at 25℃)
color: White
Stability:: Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.
CAS DataBase Reference: 81129-83-1(CAS DataBase Reference)

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Safety

RTECS: MJ9650200
HS Code: 2941.90.1050

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H319Causes serious eye irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML1283
Product name: Cilastatin sodium Ready Made Solution
Purity: 50 mg/mL in H2O
Packaging: 2ml
Price: $207
Updated: 2024/03/01

Sigma-Aldrich

Product number: C5743
Product name: Cilastatin sodium salt
Purity: ≥98%(HPLC)
Packaging: 100mg
Price: $364
Updated: 2024/03/01

Sigma-Aldrich

Product number: C2170000
Product name: Cilastatin sodium
Purity: European Pharmacopoeia (EP) Reference Standard
Packaging: c2170000
Price: $220
Updated: 2024/03/01

TCI Chemical

Product number: C3547
Product name: Cilastatin Sodium Salt
Packaging: 50MG
Price: $110
Updated: 2024/03/01

TRC

Product number: C441133
Product name: Cilastatin sodium
Packaging: 500mg
Price: $525
Updated: 2021/12/16

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Cilastatin sodium Chemical Properties,Usage,Production

Description

Cilastatin Na (81129-83-1) is a dehydropeptidase-1 inhibitor. Inhibits the proteolytic conversion of leukotriene D4?to E4.1? Inhibits the mammalian β-lactamase renal dipeptidase (dehydropeptidase-1, DPEP1) and thus is used as an antibacterial adjunct to extend the half-life of β-lactam antibiotics.2?Cilastatin also inhibits bacterial metallo-β-lactamase and thereby may block resistance to the carbapenem family of antibiotics in certain bacteria.3? Suppresses invasion and metastasis of DPEP1-expressing tumor cells.4

Chemical Properties

White or light yellow amorphous, hygroscopic powder.

Uses

Cilastatin sodium is a dipeptidase inhibitor with nephroprotective effects.

Uses

Enzyme inhibitor.

Definition

ChEBI: The monosodium salt of cilastatin. It is an inhibitor of dehydropeptidase I (membrane dipeptidase, 3.4.13.19), an enzyme found in the brush border of renal tubes and responsible for degrading the antibiotic imipenem. Cilastatin sodium is therefore administ red with imipenem to prolong the antibacterial effect of the latter by preventing its renal metabolism to microbiologically inactive and potentially nephrotoxic products.

General Description

Cilastatin sodium salt is off-white to yellowish-white, hygroscopic, amorphous compound. It is derivatized from heptenoic acid. Its molecular mass is 380.43 g.

Biological Activity

Dipeptidase inhibitor (LTDase, leukotriene D4 hydrolase, dehydropeptidase I) that displays a K i value of 0.11 μ M. Inhibits metabolism of LTD 4 to LTE 4 and the hydrolysis of β -lactam antibiotics. Nephroprotective; reduces toxic accumulation of cyclosporin A in kidney proximal tubule epithelial cells.

Biochem/physiol Actions

Inhibitor of the renal enzyme dehydropeptidase I and some bacterial zinc-containing β-lactamases. By these action, cilastatin suppresses both host and target metabolism of the broad-spectrum antibiotic imipenem, improving its efficacy.

References

1) White?et al.?(1999),?A continuous fluorometric assay for Leukotriene D4 hydrolase; Anal. Biochem.,?268?245 2) Graham?et al.?(1987),?Inhibition of the mammalian beta-lactamase renal dipeptidase (dehydropeptidase-I) by (Z)-2-acylamino-3-substituted propenoic acids; J. Med. Chem.,?30?1074 3) Keynan?et al. (1995),?The renal membrane dipeptidase (dehydropeptidase I) inhibitor, cilastatin, inhibits the bacterial metallo-beta-lactamase enzyme CphA; Antimicreob. Agents Chemother.,?39?1629 4) Park?et al.?(2016),?Dehydropeptidase 1 promotes metastasis through regulation of E-cadherin expression in colon cancer; Oncotarget,?7?9501

Cilastatin sodium Preparation Products And Raw materials

Raw materials

Preparation Products

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Cilastatin sodium Suppliers

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View Lastest Price from Cilastatin sodium manufacturers

WUHAN FORTUNA CHEMICAL CO., LTD

Product: Cilastatin sodium 81129-83-1
Price: US $0.00/KG
Min. Order: 1KG
Purity: 98%min
Supply Ability: 30tons/month
Release date: 2023-01-29

Shaanxi TNJONE Pharmaceutical Co., Ltd

Product: Cilastatin Sodium 81129-83-1
Price: US $0.00/kg
Min. Order: 1kg
Purity: 99%
Supply Ability: 10000kg
Release date: 2024-05-07

Wuhan Topule Biopharmaceutical Co., Ltd

Product: Cilastatin Sodium 81129-83-1
Price: US $11.00/g
Min. Order: 1g
Purity: 98%HPLC
Supply Ability: 20KG
Release date: 2023-06-13

81129-83-1, Cilastatin sodiumRelated Search:

Sodium benzoate Cilastatin Sodium chloride Sodium acetate N,N-Dimethylformamide Ethylbenzene Ethylparaben CHLOROETHANE Sodium carbonate Ethyl acetate Hydrogen Sodium bicarbonate Diclofenac sodium Sodium formate Ethanol Ethyl acrylate Ethyl cellulose Sodium hydroxide

2-heptenoicacid,7-((2-amino-2-carboxyethyl)thio)-2-(((2,2-dimethylcyclopropyl

l642957

monosodiumsalt,(r-(r*,s*(z)))-)carbonyl)amino)

sodium hydrogen [R-[R*,S*-(Z)]]-7-[(2-amino-2-carboxylatoethyl)thio]-2-[[(2,2-dimethylcyclopropyl)carbonyl]amino]hept-2-enoate

Cilastatine

Cilastatin sodium

Sodium 7-(2-amino-2-carboxy-ethyl)sulfanyl-2-(2,2-dimethylcyclopropyl)carbonylamino-hept-2-enoate

Sodium hydrogen 7-[(2-amino-2-carboxylatoethyl)thio]-2-[[(2,2-dimethylcyclopropyl)carbonyl]amino]hept-2-enoate

Sodium Cilastatin

[R-[R*,S*-(Z)]]-7-[(2-Amino-2-carboxyethyl)thio]-2-[[(2,2-dimethylcyclopropyl)carbonyl]amino]-2-heptenoic acid monosodium salt

(Z)-7-[(R)-2-Amino-2-carboxyethylthio]-2-[(S)-2,2-dimethylcyclopropylcarbonylamino]-2-heptenoic acid 1-sodium salt

(2Z)-7-[[(2R)-2-Amino-2-carboxyethyl]thio]-2-[[[(1S)-2,2-dimethylcyclopropyl]carbonyl]amino]-2-heptenoicacidsodiumsalt

2-Heptenoicacid,7-[[(2R)-2-aMino-2-carboxyethyl]thio]-2-[[[(1S)-2,2-diMethylcyclopropyl]carbonyl]aMino]-,sodiuM salt (1:1), (2Z)-

Cilastatin sodium Ready Made Solution

Cilastatin Impurity 9

Cilastatin sodium CRS

Cilastatin for system suitability 2 CRS

Cilastatin for system suitability 1 CRS

sodium (Z)-7-(((R)-2-amino-2-carboxyethyl)thio)-2-((S)-2,2-dimethylcyclopropanecarboxamido)hept-2-enoate

(R)-2-Amino-3-[[(Z)-6-carboxy-6-[(S)-2,2-dimethylcyclopropanecarboxamido]hex-5-en-1-yl]thio]propanoic Acid Monosodium Salt

Monosodium (R)-2-Amino-3-[[(Z)-6-carboxy-6-[(S)-2,2-dimethylcyclopropanecarboxamido]hex-5-en-1-yl]thio]propanoate

Sodium (Z)-7-(((R)-2-amino-2-carboxyethyl)thio)-2-((S)-2,2-dimethylcyclopropane-1-carboxamido)hept-2-enoate

Cilastatin sodium (C2170000)

Sod i um (Z)-7-[[(2R)-2-a mi no-2-c a rb oxye th yl]sulf a nyl]-2-[[[(1S)-2,2-d i me th ylc yc lopropyl]c a rb onyl]a mi no]h e pt-2-e noa te

Cilastatin Sodium, dehydrodipeptidase I inhibitor

81129-83-1

C16H25N2NaO5S

C16H26N2NaO5S

Miscellaneous Enzyme

APIs